WAY-181187 oxalate | CAS No. 1883548-85-3

Description

Product Description

WAY-181187 oxalate (also known as SAX-187 oxalate, CAS No. 1883548-85-3) is a synthetic, selective serotonin 5-HT6 receptor agonist. With a Ki of 2.2 nM and EC50 of 6.6 nM, it demonstrates high potency and receptor specificity. The 5-HT6 receptor is a G-protein-coupled receptor (GPCR) that plays a crucial role in modulating neurotransmission, cognition, learning, memory, and mood regulation.

Importance of 5-HT6 Receptors

• The 5-HT6 receptor is exclusively expressed in the central nervous system (CNS), particularly in the striatum, hippocampus, cortex, and nucleus accumbens.

• It is involved in cAMP-mediated signal transduction, influencing neuronal excitability and synaptic plasticity.

• Dysregulation of 5-HT6 signaling has been linked to Alzheimer’s disease, schizophrenia, depression, anxiety, and obesity.

WAY-181187 in Research

As a specific full agonist, WAY-181187 allows researchers to selectively stimulate 5-HT6 receptor signaling and study:

• Memory enhancement and learning processes.

• Cognitive dysfunction in Alzheimer’s disease.

• Mood disorders and psychiatric illnesses.

• Drug discovery for serotonin-linked pathways.

Unlike non-selective serotonin agents, WAY-181187 provides clean, receptor-specific insights into neurochemical modulation and therapeutic potential.

Broader Relevance

• Neuropharmacology: Elucidating serotonin’s contribution to cognition.

• Drug Screening: Serves as a reference agonist for testing new compounds.

• Psychiatric Research: Clarifying mechanisms underlying schizophrenia and major depressive disorder.

• Obesity Studies: Since 5-HT6 is implicated in feeding behavior, agonists may shed light on metabolic regulation.

WAY-181187 oxalate has thus become a cornerstone molecule in neuroscience and drug discovery programs.

Product Specifications

Specification Insights

• Oxalate salt form improves solubility and stability for experimental use.

• Supplied at high purity (≥98%) for consistent reproducibility.

• Compatible with both in vitro neuronal cell assays and in vivo CNS studies.

Mechanism of Action

WAY-181187 oxalate acts as a selective full agonist at the 5-HT6 receptor, which is a GPCR coupled to Gs proteins.

1. Receptor Binding

• Binds to the 5-HT6 receptor with Ki of 2.2 nM, ensuring high affinity.

• Activates receptor signaling with EC50 of 6.6 nM, confirming its role as a potent agonist.

2. Downstream Signaling Pathways

• cAMP Pathway: 5-HT6 receptor activation stimulates adenylyl cyclase, increasing cAMP levels, leading to altered neuronal excitability and gene transcription.

• Fyn Kinase Activation: Regulates synaptic plasticity, receptor trafficking, and structural neuronal changes.

• ERK1/2 Kinase Cascade: Influences memory consolidation, learning, and neurogenesis.

3. Neural Circuit Modulation

• Memory & Cognition: Enhances hippocampal and cortical plasticity, supporting memory retention.

• Mood Regulation: Impacts serotonergic tone in limbic structures, linked to anxiety and depression research.

• Neurodevelopment: May influence synaptic formation and pruning processes.

4. Research Applications in Mechanism Studies

• Provides a selective probe for dissecting serotonin pathways in CNS.

• Serves as a benchmark tool for drug discovery, allowing comparison with novel ligands.

• Supports functional MRI and behavioral models in rodents for memory and psychiatric studies.

WAY-181187 oxalate thus acts as a powerful pharmacological tool to advance knowledge of serotonin receptor biology.

Side Effects

Since WAY-181187 oxalate is for research use only, human clinical safety data is unavailable. Nevertheless, insights can be drawn from receptor pharmacology and preclinical studies:

Possible Experimental Observations

• CNS Overactivation: Excessive stimulation may alter locomotion or induce hyperactivity in animal models.

• Cognitive Imbalance: While enhancing memory at optimal doses, excessive activation may impair learning.

• Metabolic Effects: 5-HT6 receptors are implicated in appetite regulation, potentially influencing weight gain or loss.

• Mood Alterations: Could produce anxiety-like or antidepressant-like behaviors depending on dose.

Laboratory Handling Notes

• Use under BSL-2 laboratory conditions.

• Avoid unnecessary exposure; handle with gloves and protective eyewear.

• Not for diagnostic, veterinary, or therapeutic use.

These observations highlight the importance of controlled experimental dosing when using WAY-181187 oxalate.

Disclaimer

For laboratory research use only. Not approved for human or veterinary medicine.

Keywords

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